Effect of type and ratio of solubilising polymer on characteristics of hot-melt extruded orodispersible films

Low, Ariana; Parmentier, Johannes; Khong, Yuet Mei; Chai, Cherry Chang Er; Tun, Thin Yu; Berania, Jacqueline E; Liu, Xueming; Gokhale, Rajeev; Chan, Sui Yung

doi:10.1016/j.ijpharm.2013.07.046

Cited by 71 publications

(44 citation statements)

References 24 publications

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“…This could be attributed to the higher binding capacity at higher polymer concentration. Similar results were obtained by Low et al (2013) who found that the higher Soulplus Õ -containing films exhibited slower release rates. This could be due to the amphiphilic nature of Soulplus Õ which may have impeded the penetration of dissolution media (Low et al, 2013).…”

Section: In Vitro Dissolution Studysupporting

confidence: 88%

Design of freeze-dried Soluplus/polyvinyl alcohol-based film for the oral delivery of an insoluble drug for the pediatric use

Shamma

Elkasabgy

2014

Drug Delivery

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Spironolactone (SL) is a poorly water-soluble drug. Being poorly soluble affects its dissolution rate which in turn affects its oral bioavailability. This work aimed to prepare freeze-dried SL-Soluplus Õ /polyvinyl alcohol (PVA) oral thin film in an attempt to enhance the drug solubility on one hand and at the same time prepare a solid dosage form convenient for the pediatric use. SL-Soluplus Õ /PVA films were prepared using polyethylene glycol 400 (PEG 400) as a plasticizer applying the solvent-casting technique. The prepared films were evaluated for their thickness, tensile strength, and in vitro dissolution studies. Box-Behnken design (17 runs) was applied to optimize the effects of the formulation variables on the film properties. The optimized film formulation was freeze-dried after casting so as to enhance the drug dissolution. Moreover, the optimized freeze-dried film was re-characterized in vitro and evaluated in vivo in human volunteers to investigate its palatability and satisfaction. The results showed that the optimized formulation composed of 10% polymer concentration containing Soluplus Õ :PVA (0.33:0.66) and plasticized with 30% PEG 400 possessed the highest desirability value (0.836). Freeze-drying of the optimized formulation succeeded to improve SL in vitro dissolution due to the preparation of a more porous film compared to the non-freeze-dried one. In vivo evaluation of the optimized freeze-dried film showed high satisfaction among the participating volunteers concerning the ease of administration and sensation thereafter, where all the film specimens dissolved without the need for water and no film residues remained in the mouth following film dissolution. In conclusion, freeze-dried Soluplus Õ /PVA-based oral thin film proved to be a successful carrier for the oral delivery of insoluble drugs like SL for pediatrics.

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Section: In Vitro Dissolution Studysupporting

confidence: 88%

Design of freeze-dried Soluplus/polyvinyl alcohol-based film for the oral delivery of an insoluble drug for the pediatric use

Shamma

Elkasabgy

2014

Drug Delivery

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“…In onychomycosis, targeted local drug delivery via a bioadhesive film improves patient compliance because oral and other systemically administered antifungal therapies require long-term treatment, and patients often experience systemic side effects (88). In addition, the study investigated the physicochemical properties and stability of the model antifungal agent incorporated in the films (87).…”

Section: Filmsmentioning

confidence: 99%

Hot-Melt Extrusion: from Theory to Application in Pharmaceutical Formulation

2015

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Abstract. Hot-melt extrusion (HME) is a promising technology for the production of new chemical entities in the developmental pipeline and for improving products already on the market. In drug discovery and development, industry estimates that more than 50% of active pharmaceutical ingredients currently used belong to the biopharmaceutical classification system II (BCS class II), which are characterized as poorly water-soluble compounds and result in formulations with low bioavailability. Therefore, there is a critical need for the pharmaceutical industry to develop formulations that will enhance the solubility and ultimately the bioavailability of these compounds. HME technology also offers an opportunity to earn intellectual property, which is evident from an increasing number of patents and publications that have included it as a novel pharmaceutical formulation technology over the past decades. This review had a threefold objective. First, it sought to provide an overview of HME principles and present detailed engineered extrusion equipment designs. Second, it included a number of published reports on the application of HME techniques that covered the fields of solid dispersions, microencapsulation, taste masking, targeted drug delivery systems, sustained release, films, nanotechnology, floating drug delivery systems, implants, and continuous manufacturing using the wet granulation process. Lastly, this review discussed the importance of using the quality by design approach in drug development, evaluated the process analytical technology used in pharmaceutical HME monitoring and control, discussed techniques used in HME, and emphasized the potential for monitoring and controlling hot-melt technology.

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“…Tensile strength of a film is an indicator of toughness of film [17]. Etoricoxib films were cut into specimens with a width of 20 mm and a length of 60 mm.…”

Section: Mechanical Properties Of Filmsmentioning

confidence: 99%

Formulation Development of Mouth Dissolving Film of Etoricoxib for Pain Management

Senthilkumar¹,

Vijaya²

2015

Advances in Pharmaceutics

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Etoricoxib is a potent, orally active, and highly selective COX-2 inhibitor that exhibits anti-inflammatory, analgesic, and antipyretic activities. The present research was undertaken to develop mouth dissolving films of etoricoxib to have rapid onset of action. Mouth dissolving film (MDF) is a better alternate to oral disintegrating tablets due to its novelty, ease of use, and the consequent patient compliance. Solubility enhancement and taste masking of etoricoxib were the two challenges solved by formulating druginclusion complex with beta-cyclodextrin (BCD). MDF prepared by solvent casting etoricoxib-BCD complex along with HPMC as film forming polymer was found to possess desirable physicomechanical properties. In vitro release of etoricoxib from MDF in simulated salivary fluid and 0.1 N HCl was more than 95% within 2 minutes. Taste masking and in vivo disintegration were in acceptable range as assessed by human volunteers. Etoricoxib MDF was further characterized by differential scanning calorimetry, powder X-ray diffraction, and scanning electron microscopy. The index of analgesia shown by etoricoxib MDF was comparable to that of immediate release tablets (100% activity within 40 minutes) in animal studies. Conclusively, the present study documents the development of a commercially viable formula for an MDF of etoricoxib with rapidity in pain management.

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Effect of type and ratio of solubilising polymer on characteristics of hot-melt extruded orodispersible films

Cited by 71 publications

References 24 publications

Design of freeze-dried Soluplus/polyvinyl alcohol-based film for the oral delivery of an insoluble drug for the pediatric use

Design of freeze-dried Soluplus/polyvinyl alcohol-based film for the oral delivery of an insoluble drug for the pediatric use

Hot-Melt Extrusion: from Theory to Application in Pharmaceutical Formulation

Formulation Development of Mouth Dissolving Film of Etoricoxib for Pain Management

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